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The selectivity inhibition method of Janus tyrosine kinase 3 (JAK3)

机译:Janus酪氨酸激酶3(JAK3)的选择性抑制方法

摘要

Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.
机译:公开了抑制或破坏淋巴细胞或骨髓来源的细胞中Janus酪氨酸激酶3(Jak3)依赖性功能,特别是阻断淋巴细胞(例如T细胞,B细胞)增殖和功能的方法。使用曼尼希碱化合物或其衍生物或修饰的化合物,该化合物能够选择性地抑制Jak3,同时以较小的程度或根本不影响其他蛋白质酪氨酸激酶的活性,从而提供有益的效果,例如减轻移植排斥和缓解比传统的免疫抑制剂具有更少的副作用的过敏反应。

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